| 货号 | 16423-1mg |
| 描述 | The Pim family proteins are serine/threonine kinases involved in cancer progression.1 SGI-1776 is a potent inhibitor of all three human Pim kinases (IC50s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively).2 While it also inhibits FLT3 and haspin (IC50s = 44 and 34 nM, respectively), SGI-1776 has little effect on several other kinases, including cell cycle kinases.2 SGI-1776 induces apoptosis in lymphocytes from patients with chronic or acute lymphocytic leukemia but not in those from healthy donors.2,3 At 10 µM, it reduces STAT3 phosphorylation without reducing STAT3 expression in cancer cells, and this correlates with inhibition of cell proliferation.4 SGI-1776 also enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant prostate cancer cells to taxanes.5,6 |
| 别名 | Pim-Kinase Inhibitor IX; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Beharry, Z.,Mahajan, S.,Zemskova, M., et al. The Pim protein kinases regulate energy metabolism and cell growth. Proceedings of the National Academy of Sciences of the United States of America 108(2), 528-533 (2011). 2.Chen, L.S.,Redkar, S.,Bearass, D., et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells. Blood 114(19), 4150-4157 (2009). 3.Chen, L.S.,Redkar, S.,Taverna, P., et al. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood 118(3), 693-702 (2011). 4.Chang, M.,Kanwar, N.,Feng, E., et al. PIM kinase inhibitors downregulate STAT3Tyr705 phosphorylation. Molecular Cancer Therapeutics 9(9), 2478-2487 (2010). 5.Mahalingam, D.,Espitia, C.M.,Medina, E.C., et al. Targeting PIM kinase enhances the activity of sunitinib in renal cell carcinoma. British Journal of Cancer 105(10), 1563-1573 (2011). 6.Mumenthaler, S.M.,Ng, P.Y.B.,Hodge, A., et al. Pharmacologic inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes. Molecular Cancer Therapeutics 8(10), 2882-2893 (2009). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 405.4 |
| 分子式 | C20H22F3N5O |
| CAS号 | 1025065-69-3 |
| 稳定性 | ≥ 2 years |
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